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1038395-65-1 (KX2-391 (dihydrochloride))

1

Identification

KX2-391 (dihydrochloride) KX2-391 (dihydrochloride)
Name KX2-391 (dihydrochloride)
Formula C26H31Cl2N3O3
MW 504.45
CAS No. 1038395-65-1
EINECS
Smiles O=C(CC1=NC=C(C2=CC=C(OCCN3CCOCC3)C=C2)C=C1)NCC4=CC=CC=C4.Cl.Cl
Synonyms KX2-391 2HCl; KX2-391; N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide dihydrochloride
InChI InChI=1S/C26H29N3O3.2ClH/c30-26(28-19-21-4-2-1-3-5-21)18-24-9-6-23(20-27-24)22-7-10-25(11-8-22)32-17-14-29-12-15-31-16-13-29;;/h1-11,20H,12-19H2,(H,28,30);2*1H
2

Introduction

KX2-391 2Hcl (KX01) is the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

Background Information

KX2-391 2Hcl is the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. ......by AdooQ BioScience, LLC
KX2-391 2Hcl is the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. ......by BOC Sciences
KX-392 is a potent oral non-ATP competitive inhibitor of Src kinase and tubulin polymerization. KX2-391 shows steep dose-response curves against Huh7 (GI₅₀ = 9 nM), PLC/PRF/5 (GI₅₀ = 13 nM), Hep3B (GI₅₀ = 26 nM), and HepG2 (GI₅₀ = 60 nM), four hepatic cell cancer (HCC) cell lines. ......by BioVision, Inc.,
KX2-391 (dihydrochloride) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. ......by MedChemexpress Co., Ltd.
A highly selective, non-ATP competitive substrate-pocket-directed Src/pretubulin inhibitor; inhibits c-Src kinase with GI50s of 1.34 uM and 2.30 μM in NIH3T3/c-Src527F and SYF/c-Src527F cells, respectively; causes microtubule disruption in tumor cells; orally active.Solid TumorsPhase 2 Clinical ......by ProbeChem
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:White to off-white solid EBNumber:EB000028711

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
KX2-391 (dihydrochloride) Kinex Pharmaceuticals Corp Hormone refractory prostate cancer 2010/2/28 2012/8/31 Phase 2 Clinical
KX2-391 (dihydrochloride) Hanmi Pharmaceutical Co Ltd Advanced solid tumor 2012/12/31 2016/5/31 Phase 2 Clinical
KX2-391 (dihydrochloride) Kinex Pharmaceuticals Corp Acute myelogenous leukemia 2011/7/31 2013/10/31 Phase 1 Clinical
KX2-391 (dihydrochloride) Kinex Pharmaceuticals Corp Lymphoma 2007/11/30 2011/5/31 Phase 1 Clinical
KX2-391 (dihydrochloride) Kinex Pharmaceuticals Corp Solid tumor 2007/11/30 2011/5/31 Phase 1 Clinical
KX2-391 (dihydrochloride) - Phase 2
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Safety Data of KX2-391 (dihydrochloride)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
BioVision, Inc., USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD84();10mg/USD144() USA
MedChemexpress Co., Ltd. 5mg/USD84();10mg/USD144() USA
ProbeChem
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD84();10mg/USD144() China
10

Related Products

Other Forms of 1038395-65-1

Name CAS No Formula MW
KX2-391 897016-82-9 C26H29N3O3 431.53
KX2-391 (Mesylate) 1080645-95-9 C27H33N3O6S 527.6324

Recommended Compounds in Src Microtubule/Tubulin

Name CAS No Formula MW
Scutellarein 529-53-3 C15H10O6 286.24
A 419259 (trihydrochloride) 1435934-25-0 C29H37Cl3N6O 592.0
A 419259 364042-47-7 C29H34N6O 482.62
1-Naphthyl PP1 221243-82-9 C19H19N5 317.39
XL228 898280-07-4 C22H31N9O 437.54
Dasatinib (hydrochloride) 854001-07-3 C22H27Cl2N7O2S 524.47
MNS 1485-00-3 C9H7NO4 193.15618
PP2 172889-27-9 C15H16ClN5 301.77
PP1 172889-26-8 C16H19N5 281.36
ZM 306416 690206-97-4 C16H13ClFN3O2 333.74
AMG-47a 882663-88-9 C29H28F3N5O2 535.56
KX1-004 518058-84-9 C16H13FN2O2 284.29
AZM475271 476159-98-5 C23H27ClN4O3 442.9385
DCC-2036 1020172-07-9 C30H28FN7O3 553.59
Lck Inhibitor 847950-09-8 C31H30N8O 530.62
Lck inhibitor 2 944795-06-6 C18H17N5O2 335.36
PD173955 260415-63-2 C21H16Cl2N4OS 443.35
TG 100801 (Hydrochloride) 1018069-81-2 C33H31Cl2N5O3 616.54
TG 100801 867331-82-6 C33H30ClN5O3 580.08
TG 100572 (Hydrochloride) 867331-64-4 C26H27Cl2N5O2 512.43

Recommended Compounds in Same Indication

Name CAS No Formula MW
AZD1152 722543-31-9 C26H31FN7O6P 587.54
AZD1152-HQPA 722544-51-6 C26H30FN7O3 507.56
Mocetinostat 726169-73-9 C23H20N6O 396.44
OSI-930 728033-96-3 C22H16F3N3O2S 443.44
TAK-700 (R-form) 752243-39-3 C18H17N3O2 307.35
Volasertib 755038-65-4 C34H50N8O3 618.81
Olaparib 763113-22-0 C24H23FN4O3 434.46
AT7867 857531-00-1 C20H20ClN3 337.85
NVP-BGJ398 872511-34-7 C26H31Cl2N7O3 560.48
PU-H71 873436-91-0 C18H21IN6O2S 512.37
BMS-599626 (Hydrochloride) 873837-23-1 C27H28ClFN8O3 567.01
RO4987655 874101-00-5 C20H19F3IN3O5 565.28
MGCD-265 analog 875337-44-3 C26H20FN5O2S2 517.5977
Regorafenib (Hydrochloride) 835621-07-3 C21H16Cl2F4N4O3 519.28
AT9283 896466-04-9 C19H23N7O2 381.43
KX2-391 897016-82-9 C26H29N3O3 431.53
Bicalutamide 90357-06-5 C18H14F4N2O4S 430.37
Bleomycin (sulfate) 9041-93-4 C110H168N34O46S7 2927.17
MLN4924 905579-51-3 C21H25N5O4S 443.52
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
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Route of Synthesis

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References

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More Information

KX2-391 (dihydrochloride)

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